Metoclopramidum

General characteristics. Structure:

Active agent: 10 mg of Metoclopramidum of a hydrochloride in 1 ampoule.

Excipients: sodium pyrosulphite, sodium chloride, water for injections.

Pharmacological properties:

Pharmacodynamics. The specific blocker of dopamine (D2) and serotoninovy (5-NTZ) receptors, oppresses chemoceptors of a trigger zone of a brainstem, weakens sensitivity of the visceral nerves transferring impulses from a pylorus and a duodenum to the emetic center. Through a hypothalamus and a parasympathetic nervous system (a GIT innervation) exerts the regulating and coordinating impact on a tone and a physical activity of an upper part of a GIT (including a tone of the lower sphincter of a gullet). Raises a tone of a stomach and intestines, accelerates gastric emptying, reduces hyperacid стаз, interferes with a peloric and ezofagealny reflux, stimulates an intestines peristaltics.

Normalizes department of bile, reduces a spasm of the Sphincter of Oddi. Without changing its tone, eliminates dyskinesia of a gall bladder. Does not possess M-holinoblokiruyushchim, antihistaminic, antiserotoninovy and ganglioblokiruyushchy action; kidneys and a liver, on blood formation, secretion of a stomach and pancreas do not influence a tone of blood vessels of a brain, arterial pressure, breath function, and also. Stimulates prolactin secretion. Increases sensitivity of fabrics to acetylcholine (action does not depend on a vagal innervation, but is eliminated with holinoblokator). Stimulating secretion of Aldosteronum, strengthens Na delay ⁺ and removal ^{of K+}.

The beginning of action on digestive tract is noted in 1 – 3 minutes later in/in introductions and in 10 – 15 minutes after introduction in oil and is shown by acceleration of evacuation of contents of a stomach and antiemetic effect.

Is exposed to metabolism in a liver. Removal of drug happens generally through kidneys within 24 – 72 hours (85% of a dose), 30% in an invariable look. Easily gets through placental and hematoencephalic barriers, it is allocated with breast milk.

Indications to use:

Vomiting, nausea, hiccups of various genesis (it can be in certain cases effective at the vomiting caused by radiation therapy or reception of tsitostatik). Atony and hypotonia of a stomach and intestines (in particular, postoperative); dyskinesia of biliary tract; reflux esophagitis; meteorism; as a part of complex therapy of aggravations of a peptic ulcer of a stomach and a duodenum. It is applied to strengthening of a vermicular movement when carrying out X-ray contrast researches of digestive tract.

Route of administration and doses:

Enter in/in or in oil the adult in a dose of 10 - 20 mg of 1 - 3 time a day (the maximum daily dose – 60 mg); to children 6 years of 2,5 - 5 mg of 1 - 3 time a day are more senior; for children aged from 2 to 6 years the daily dose makes 0,5 – 1 mg/kg of body weight, frequency rate of introduction of 1 - 3 time.

For prevention and treatment of nausea and the vomiting caused by reception of tsitostatik or radiation therapy, the drug is administered intravenously in a dose of 2 mg/kg of body weight in 30 minutes prior to use of tsitostatik or radiation; if necessary introduction is repeated in 2 – 3 hours.

Before X-ray inspection adult enter intravenously 10 – 20 mg in 5 – 15 min. prior to the research.

The patient with clinically expressed hepatonephric insufficiency at the beginning appoint a dose twice smaller usual, the subsequent dose depends on individual reaction of the patient to Metoclopramidum.

Features of use:

It is not effective at vomiting of vestibular genesis. Do not appoint after digestive tract operations (as a pyloroplasty or an anastomosis of intestines) as vigorous muscular contractions interfere with healing.

Against the background of use of Metoclopramidum distortions of these laboratory indicators of function of a liver and definition of concentration of Aldosteronum and prolactin in plasma are possible.

At administration of drug it is necessary to avoid potentially dangerous types of activity requiring special attention, bystry mental and motor reaction (control of vehicles, etc.).

The majority of side effects arise within 36 hours from an initiation of treatment and disappear within 24 hours after cancellation. Treatment has to be whenever possible short-term.

During treatment by drug alcohol intake is not recommended.

Pregnancy and lactation. Use of Metoclopramidum in the period of a lactation is not recommended, in need of use of drug it is necessary to resolve an issue of the breastfeeding termination.

Side effects:

From a nervous system: extrapyramidal frustration – a spasm of facial muscles, a lockjaw, a rhythmic protrusion of language, bulbar type of the speech, a spasm of extraocular muscles (including okulogirny crisis), a spastic wryneck, an opisthotonos, a muscle hyper tone; parkinsonism (a hyperkinesia, muscular rigidity – manifestation dopamine - the blocking action, the risk of development in children and teenagers increases at exceeding of a dose of 0,5 mg/Civil Code/days); dyskineses (at elderly, at a chronic renal failure); drowsiness, fatigue, depression, uneasiness, confusion, headache, sonitus.

From the alimentary system: a lock or diarrhea, it is rare – dryness in a mouth.

Allergic reactions: small tortoiseshell.

From endocrine system: seldom (at long reception in high doses) – a gynecomastia, a galactorrhoea, disturbance of a menstrual cycle.

Others: in an initiation of treatment the agranulocytosis is possible, it is rare (at use in high doses) — a hyperemia of a mucous membrane of a nose.

Interaction with other medicines:

Strengthens effect of ethanol on the central nervous system, sedation of hypnagogues, efficiency of therapy H2-gistaminoblokatorami.

Increases absorption of tetracycline, ampicillin, paracetamol, acetylsalicylic acid, a levodopa, ethanol; slows down absorption of a digogsin and Cimetidinum.

It is not necessary to appoint along with neuroleptics since the risk of emergence of extrapyramidal reactions increases.

At simultaneous use with neuroleptics the risk of development of extrapyramidal symptoms increases.

Antikholinesterazny means can weaken action of Metoclopramidum.

Contraindications:

Bleedings from digestive tract, a pyloric stenosis, mechanical intestinal impassability, perforation of a stomach or intestines, a pheochromocytoma, epilepsy, glaucoma, extrapyramidal disturbances, Parkinson's disease, prolaktinozavisimy tumors, vomiting against the background of treatment or overdose by neuroleptics and at patients with cancer of a mammary gland, pregnancy (the I trimester), the lactation period, early children's age (up to 2 years), hypersensitivity to Metoclopramidum or other components of drug.

With care – children's age, advanced age, a renal/liver failure, bronchial asthma, arterial hypertension.

Overdose:

The hypersomnia, disorientation and extrapyramidal frustration can be noted. As a rule, the symptomatology disappears after the termination of administration of drug within 24 hours. If necessary treatment is carried out by holinoblokator and protivoparkinsonichesky means.

Storage conditions:

To store in the place protected from light at a temperature below 25 ºС. To store in the place, unavailable to children. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

Solution for intravenous and intramuscular administration of 5 mg/ml. On 2 ml in ampoules from colourless hydrolytic glass I of a class. On an ampoule the color ring in the place of a break is put. On 5 ampoules place in a blister strip packaging. On 1 blister strip packaging together with the application instruction place in a cardboard pack.